Rational design, synthesis, and serine protease inhibitory activity of novel P-1-argininoyl heterocycles

被引：23
|
作者：
Tamura, SY
Shamblin, BM
Brunck, TK
Ripka, WC
机构：
[1] Department of Medicinal Chemistry, Corvas International, Inc., San Diego, CA 92121
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 10期
关键词：
D O I：
10.1016/S0960-894X(97)00227-8
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Peptidomimetic derivatives featuring a P-1-argininoyl heterocycle were designed. The preparation of two key building blocks containing benzoxazole or benzimidazole rings and their incorporation into thrombin and factor Xa specific sequences is described. The serine protease inhibitory activity of these targets was evaluated. Molecular modeling of two representative structures is presented. (C) 1997 Elsevier Science Ltd.
引用
收藏
页码：1359 / 1364
页数：6
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